摘要
DNA 被包装在组蛋白的八聚体中,形成染色质,即 DNA 和蛋白质的复合物。染色体的结构基质、染色质及其变化现在被认为是控制基因表达的重要因素,这激发了人们对了解控制各种疾病(包括癌症)的遗传途径的兴趣。作为转录沉默机制的 CpG 二核苷酸中的 DNA 甲基化、翻译后组蛋白修饰(例如乙酰化、甲基化和其他影响染色质结构、ATP 依赖性染色质重塑和 miRNA 介导的基因沉默)都被发现在各种癌症的类型。在这篇综述中,我们分析了基因表达的主要改变、癌细胞中的表观遗传修饰模式、每种表观遗传机制的主要调节剂和抑制剂,以及最具代表性的抑制剂的分子进化,所有这些都指向了 HAT 的广阔前景、HDAC、非糖苷类 DNMT 抑制剂和结构域抑制剂。
关键词: 癌症、染色质、组蛋白、DNA、表观遗传抑制剂、表观基因瘤。
Current Medicinal Chemistry
Title:Epigenetic Modulators as Treatment Alternative to Diverse Types of Cancer
Volume: 29 Issue: 9
关键词: 癌症、染色质、组蛋白、DNA、表观遗传抑制剂、表观基因瘤。
摘要: DNA is packaged in an octamer of histones, forming chromatin, a complex of DNA and proteins. The structural matrix of a chromosome, chromatin and its changes are now regarded as important factors in controlling gene expression, which has sparked a lot of interest in understanding genetic pathways governing various diseases, including cancer. DNA methylation in the CpG dinucleotide as a transcriptional silencing mechanism, post-translational histone modifications such as acetylation, methylation, and others that affect chromatin structure, ATP-dependent chromatin remodelling, and miRNA-mediated gene silencing are all found to be important in various types of cancer. In this review, we analyze the main alterations in gene expression, epigenetic modification patterns in cancer cells, the main modulators and inhibitors of each epigenetic mechanism, and the molecular evolution of the most representative inhibitors, all of which point to a promising future for HAT, HDAC, non-glycoside DNMT inhibitors, and domain inhibitors.
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Epigenetic Modulators as Treatment Alternative to Diverse Types of Cancer, Current Medicinal Chemistry 2022; 29 (9) . https://dx.doi.org/10.2174/0929867329666211228111036
DOI https://dx.doi.org/10.2174/0929867329666211228111036 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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